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LU-32-176B

Names

[ CAS No. ]:
770688-66-9

[ Name ]:
LU-32-176B

Biological Activity

[Description]:

LU-32-176B, a GABA transporter 1(GAT1) selective inhibitor, is found to exert a synergistic anticonvulsant action with GAT2 transport inhibitor EF1502. LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Membrane Transporter/Ion Channel >> GABA Receptor
Signaling Pathways >> Neuronal Signaling >> GABA Receptor

[Target]

LU-32-176B inhibits neurons, astrocytes and mGAT1 with the IC50 values of 2μM, 1μM, 4μM, respectively[1][2].


[In Vivo]

LU-32-176B (i.p.) and EF1502 can prevent sound-induced seizures in the Frings AGS-susceptible mouse model[1].

[References]

[1]. Schousboe A, et al. GABA transporters as drug targets for modulation of GABAergic activity. Biochem Pharmacol. 2004;68(8):1557-1563.

[2]. White HS, et al. First demonstration of a functional role for central nervous system betaine/{gamma}-aminobutyric acid transporter (mGAT2) based on synergistic anticonvulsant action among inhibitors of mGAT1 and mGAT2. J Pharmacol Exp Ther. 2005;312(2):866-874.

Chemical & Physical Properties

[ Molecular Formula ]:
C23H24F2N2O2

[ Molecular Weight ]:
398.45

Safety Information

[ Hazard Codes ]:
Xi

Related Compounds